Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T31424 | Target Info | |||
Target Name | Adrenergic receptor Alpha-2 (ADRA2) | ||||
Synonyms |
Alpha-2 adrenergic receptor; Alpha(2)-adrenoceptor
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Target Type | Successful Target | ||||
Gene Name | NO-GeName | ||||
Biochemical Class | GPCR rhodopsin | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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Co-Target Name | Adrenergic receptor alpha-1D (ADRA1D) | Successful Target | ||||
UniProt ID | ADA1D_HUMAN | |||||
Gene Name | ADRA1D | |||||
Synonyms |
Alpha-adrenergic receptor 1a; Alpha-1D adrenoreceptor; Alpha-1D adrenoceptor; Alpha-1D adrenergic receptor; Alpha adrenergic receptor 1a; Alpha 1D-adrenoreceptor; Alpha 1D-adrenoceptor; ADRA1A
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Representative Drug(s) | Dexmedetomidine | Drug Info | Ki = 0.015 nM | Click to Show More | [1] | |
2 | Yohimbine | Drug Info | Ki = 1.6 nM | [3] | ||
3 | Guanabenz | Drug Info | Ki = 232 nM | [6] | ||
4 | Clonidine | Drug Info | Ki = 595 nM | [6] | ||
5 | Brimonidine | Drug Info | Ki = 933.25 nM | [14] | ||
Co-Target Name | 5-HT 1B receptor (HTR1B) | Successful Target | ||||
UniProt ID | 5HT1B_HUMAN | |||||
Gene Name | HTR1B | |||||
Synonyms |
Serotonin receptor 1B; Serotonin 1D beta receptor; S12; HTR1DB; 5-hydroxytryptamine receptor 1B; 5-HT1B receptor; 5-HT1B; 5-HT-1D-beta; 5-HT-1B
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Representative Drug(s) | Oxymetazoline | Drug Info | Ki = 0.3 nM | [2] | ||
Co-Target Name | 5-HT 1D receptor (HTR1D) | Successful Target | ||||
UniProt ID | 5HT1D_HUMAN | |||||
Gene Name | HTR1D | |||||
Synonyms |
Serotonin receptor 1D; Serotonin 1D alpha receptor; HTRL; HTR1DA; 5HT1D; 5-hydroxytryptamine receptor 1D; 5-HT1D receptor; 5-HT1D; 5-HT-1D-alpha; 5-HT-1D
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Representative Drug(s) | Oxymetazoline | Drug Info | Ki = 0.4 nM | [2] | ||
Co-Target Name | Adrenergic receptor alpha-1B (ADRA1B) | Successful Target | ||||
UniProt ID | ADA1B_HUMAN | |||||
Gene Name | ADRA1B | |||||
Synonyms |
Alpha-1B adrenoreceptor; Alpha-1B adrenoceptor; Alpha-1B adrenergic receptor; Alpha 1B-adrenoreceptor; Alpha 1B-adrenoceptor
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Representative Drug(s) | Yohimbine | Drug Info | Ki = 1.1 nM | Click to Show More | [3] | |
2 | Oxymetazoline | Drug Info | Ki = 831.76 nM | [5] | ||
Co-Target Name | Debrisoquine 4-hydroxylase (CYP2D6) | Successful Target | ||||
UniProt ID | CP2D6_HUMAN | |||||
Gene Name | CYP2D6 | |||||
Synonyms |
P450-DB1; Cytochrome P450-DB1; Cytochrome P450 2D6; CYPIID6; CYP2DL1
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Representative Drug(s) | Yohimbine | Drug Info | IC50 = 8.4 nM | Click to Show More | [4] | |
2 | Oxymetazoline | Drug Info | IC50 = 200 nM | [6] | ||
Co-Target Name | Adrenergic receptor alpha-1A (ADRA1A) | Successful Target | ||||
UniProt ID | ADA1A_HUMAN | |||||
Gene Name | ADRA1A | |||||
Synonyms |
Alpha-adrenergic receptor 1c; Alpha-1C adrenergic receptor; Alpha-1A adrenoreceptor; Alpha-1A adrenoceptor; Alpha-1A adrenergic receptor; Alpha adrenergic receptor 1c; Alpha 1A-adrenoreceptor; Alpha 1A-adrenoceptor; ADRA1C
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Representative Drug(s) | Oxymetazoline | Drug Info | Ki = 15.85 nM | Click to Show More | [5] | |
2 | Clonidine | Drug Info | Ki = 512.86 nM | [13] | ||
Co-Target Name | 5-HT 2B receptor (HTR2B) | Successful Target | ||||
UniProt ID | 5HT2B_HUMAN | |||||
Gene Name | HTR2B | |||||
Synonyms |
Serotonin receptor 2B; 5-hydroxytryptamine receptor 2B; 5-HT2B; 5-HT-2B; 5-HT 2B
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Representative Drug(s) | Yohimbine | Drug Info | Ki = 47 nM | Click to Show More | [6] | |
2 | Guanabenz | Drug Info | Ki = 62 nM | [6] | ||
Co-Target Name | Trace amine-associated receptor-1 (TAAR1) | Successful Target | ||||
UniProt ID | TAAR1_HUMAN | |||||
Gene Name | TAAR1 | |||||
Synonyms |
Trace amine receptor 1; TaR-1; TAAR1
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Representative Drug(s) | Guanabenz | Drug Info | EC50 = 90 nM | [7] | ||
Co-Target Name | Monoamine oxidase (MAO) | Successful Target | ||||
UniProt ID | AOFA_HUMAN; AOFB_HUMAN | |||||
Gene Name | NO-GeName | |||||
Synonyms |
Human monoamine oxidase
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Representative Drug(s) | Clonidine | Drug Info | Ki ~ 100 nM | [8] | ||
Co-Target Name | 5-HT 2C receptor (HTR2C) | Successful Target | ||||
UniProt ID | 5HT2C_HUMAN | |||||
Gene Name | HTR2C | |||||
Synonyms |
Serotonin receptor 2C; HTR1C; 5HT-1C; 5-hydroxytryptamine receptor 2C; 5-hydroxytryptamine receptor 1C; 5-HTR2C; 5-HT2C receptor; 5-HT2C; 5-HT1C; 5-HT-2C; 5-HT-1C
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Representative Drug(s) | Guanabenz | Drug Info | Ki = 107 nM | Click to Show More | [6] | |
2 | Oxymetazoline | Drug Info | Ki = 303 nM | [6] | ||
Co-Target Name | 5-HT 2A receptor (HTR2A) | Successful Target | ||||
UniProt ID | 5HT2A_HUMAN | |||||
Gene Name | HTR2A | |||||
Synonyms |
Serotonin receptor 2A; HTR2; 5-hydroxytryptamine receptor 2A; 5-HT-2A; 5-HT-2
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Representative Drug(s) | Guanabenz | Drug Info | Ki = 112 nM | Click to Show More | [6] | |
2 | Oxymetazoline | Drug Info | Ki = 367 nM | [6] | ||
Co-Target Name | 5-HT 1A receptor (HTR1A) | Successful Target | ||||
UniProt ID | 5HT1A_HUMAN | |||||
Gene Name | HTR1A | |||||
Synonyms |
Serotonin receptor 1A; G-21; ADRBRL1; ADRB2RL1; 5-hydroxytryptamine receptor 1A; 5-HT1A receptor; 5-HT1A; 5-HT-1A
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Representative Drug(s) | Lofexidine | Drug Info | Ki = 125.89 nM | [9] | ||
Co-Target Name | Opioid receptor mu (MOP) | Successful Target | ||||
UniProt ID | OPRM_HUMAN | |||||
Gene Name | OPRM1 | |||||
Synonyms |
hMOP; Mu-type opioid receptor; Mu opioid receptor; Mu opiate receptor; MOR1A; MOR1; MOR-1; M-OR-1
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Representative Drug(s) | Meperidine | Drug Info | IC50 = 315 nM | [10] | ||
Co-Target Name | Voltage-gated potassium channel Kv11.1 (KCNH2) | Successful Target | ||||
UniProt ID | KCNH2_HUMAN | |||||
Gene Name | KCNH2 | |||||
Synonyms |
hERG1; hERG-1; Voltage-gated potassium channel subunit Kv11.1; Potassium voltage-gated channel subfamily H member 2; HERG K+ channel; HERG; H-ERG; Ether-a-go-go-related protein 1; Ether-a-go-go-related gene potassium channel 1; Ether-a-go-go related protein 1; Ether-a-go-go related gene potassium channel 1; Eag related protein 1; Eag homolog; ERG-1; ERG
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Representative Drug(s) | Meperidine | Drug Info | IC50 = 323.59 nM | [11] | ||
Co-Target Name | Muscarinic acetylcholine receptor M4 (CHRM4) | Successful Target | ||||
UniProt ID | ACM4_HUMAN | |||||
Gene Name | CHRM4 | |||||
Synonyms |
M4 receptor; CHRM4
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Representative Drug(s) | Oxymetazoline | Drug Info | Ki = 455 nM | [6] | ||
Co-Target Name | Opioid receptor delta (OPRD1) | Successful Target | ||||
UniProt ID | OPRD_HUMAN | |||||
Gene Name | OPRD1 | |||||
Synonyms |
OPRD; Delta-type opioid receptor; Delta opioid receptor; DOR-1; D-OR-1
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Representative Drug(s) | Meperidine | Drug Info | IC50 = 500 nM | [12] | ||
Co-Target Name | Opioid receptor kappa (OPRK1) | Successful Target | ||||
UniProt ID | OPRK_HUMAN | |||||
Gene Name | OPRK1 | |||||
Synonyms |
OPRK; Kappa-type opioid receptor; Kappa opioid receptor; KOR-1; KOR; K-OR-1
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Representative Drug(s) | Meperidine | Drug Info | IC50 = 500 nM | [12] | ||
Co-Target Name | Dopamine D2 receptor (D2R) | Successful Target | ||||
UniProt ID | DRD2_HUMAN | |||||
Gene Name | DRD2 | |||||
Synonyms |
Dopamine receptor 2; D(2) dopamine receptor
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Representative Drug(s) | Yohimbine | Drug Info | Ki = 687 nM | [6] | ||
Co-Target Name | Muscarinic acetylcholine receptor M5 (CHRM5) | Successful Target | ||||
UniProt ID | ACM5_HUMAN | |||||
Gene Name | CHRM5 | |||||
Synonyms |
CHRM5
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Representative Drug(s) | Oxymetazoline | Drug Info | Ki = 957 nM | [6] | ||
Co-Target Name | 5-HT 6 receptor (HTR6) | Clinical trial Target | ||||
UniProt ID | 5HT6R_HUMAN | |||||
Gene Name | HTR6 | |||||
Synonyms |
Serotonin receptor 6; 5-hydroxytryptamine receptor 6; 5-HT6 receptor; 5-HT6; 5-HT-6
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Representative Drug(s) | Oxymetazoline | Drug Info | Ki = 775 nM | Click to Show More | [6] | |
2 | Yohimbine | Drug Info | Ki = 784 nM | [6] | ||
Co-Target Name | Imidazoline receptor 1 (IR1) | Literature-reported Target | ||||
UniProt ID | NISCH_HUMAN | |||||
Gene Name | NISCH | |||||
Synonyms |
hIRAS; KIAA0975; Imidazoline-1 receptor candidate protein; Imidazoline-1 receptor; Imidazoline receptor antisera-selected protein; IRAS; IR1; I1R candidate protein; I-1 receptor candidate protein; I-1
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Representative Drug(s) | Oxymetazoline | Drug Info | Ki = 6.194 nM | Click to Show More | [15] | |
2 | Clonidine | Drug Info | Ki = 8.9 nM | [16] | ||
3 | Tizanidine | Drug Info | Ki = 28.3 nM | [15] | ||
4 | Guanabenz | Drug Info | Ki = 34.67 nM | [15] | ||
Co-Target Name | HUAMN alpha-1 adrenergic receptor (ADRA1) | Literature-reported Target | ||||
UniProt ID | ADA1A_HUMAN; ADA1B_HUMAN; ADA1D_HUMAN | |||||
Gene Name | ADRA1A; ADRA1B; ADRA1D | |||||
Synonyms |
Alpha-1 adrenoreceptor
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Representative Drug(s) | Apraclonidine | Drug Info | EC50 = 180 nM | Click to Show More | [17] | |
2 | Clonidine | Drug Info | EC50 = 290 nM | [17] | ||
Co-Target Name | Solute carrier family 22 member 1 (SLC22A1) | Co-Target | ||||
UniProt ID | S22A1_HUMAN | |||||
Gene Name | SLC22A1 | |||||
Synonyms |
Organic cation transporter 1; hOCT1
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Representative Drug(s) | Clonidine | Drug Info | Ki = 550 nM | [18] |
References | Top | ||||
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REF 1 | Alpha(2) adrenoceptor agonists as potential analgesic agents. 3. Imidazolylmethylthiophenes. J Med Chem. 2001 Mar 15;44(6):863-72. | ||||
REF 2 | Benzylimidazolines as h5-HT1B/1D serotonin receptor ligands: a structure-affinity investigation. J Med Chem. 1998 Jun 18;41(13):2243-51. | ||||
REF 3 | Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification. J Med Chem. 1995 Sep 1;38(18):3415-44. | ||||
REF 4 | Validation of model of cytochrome P450 2D6: an in silico tool for predicting metabolism and inhibition. J Med Chem. 2004 Oct 21;47(22):5340-6. | ||||
REF 5 | 2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: the discovery of alpha1a subtype selective 2'-alkylsulfonyl-substituted analogues. J Med Chem. 2002 May 23;45(11):2229-39. | ||||
REF 6 | DrugMatrix in vitro pharmacology data. National Toxicology Program | ||||
REF 7 | Discovery of trace amine-associated receptor 1 ligands by molecular docking screening against a homology model. Medchemcomm. 2015;6:2216-23. | ||||
REF 8 | Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications. J Med Chem. 1995 Sep 15;38(19):3681-716. | ||||
REF 9 | Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect. ACS Med Chem Lett. 2012 Jun 8;3(7):535-9. | ||||
REF 10 | From hit to lead. Combining two complementary methods for focused library design. Application to mu opiate ligands. J Med Chem. 2001 Oct 11;44(21):3378-90. | ||||
REF 11 | A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors. Bioorg Med Chem Lett. 2005 Jun 2;15(11):2886-90. | ||||
REF 12 | Synthesis and biological activity of fluoroalkylamine derivatives of narcotic analgesics. J Med Chem. 1980 Sep;23(9):985-90. | ||||
REF 13 | A convenient synthesis of 2-amino-2-oxazolines and their pharmacological evaluation at cloned human alpha adrenergic receptors. Bioorg Med Chem Lett. 1994 Oct 6;4(19):2317-22. | ||||
REF 14 | Pharmacological evaluation of UK-14,304 analogs at cloned human alpha adrenergic receptors. Bioorg Med Chem Lett. 1995 Oct 5;5(19):2255-8. | ||||
REF 15 | QSAR study of imidazoline antihypertensive drugs. Bioorg Med Chem. 2008 Aug 1;16(15):7134-40. | ||||
REF 16 | Synthesis and pharmacologic evaluation of 2-endo-amino-3-exo-isopropylbicyclo[2.2.1]heptane: a potent imidazoline1 receptor specific agent. J Med Chem. 1996 Mar 15;39(6):1193-5. | ||||
REF 17 | Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist. J Med Chem. 1996 Aug 30;39(18):3533-8. | ||||
REF 18 | Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa). J Pharmacol Exp Ther. 1998 Jul;286(1):354-61. |
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